The document discusses aminoglycoside antibiotics such as gentamicin and amikacin. It describes their mechanisms of action as inhibiting protein synthesis, administration via injection except for neomycin, and potential adverse effects including nephrotoxicity and ototoxicity. It also lists their uses in treating various infections and important drug interactions to be aware of when prescribing aminoglycosides.

1. PATIENT PROFILE & PATIENT COUNSELING
C. DRUG PROFILE OF ATLEAST 25 IMPORTANT
MEDICATIONS
2. AMINOGLYCOSIDES
CLINICAL PHARMACY
BY
Zul Kamal
DEPARTMENT OF PHARMACY
SHAHEED BENAZIR BHUTTO UNIVERSITY,
SHERINGAL

2. C. DRUG PROFILE OF ATLEAST 25 IMPORTANT MEDICATIONS
MECHANISMS OF ACTION OF ANTIBACTERIAL DRUGS
1. Inhibit cell wall synthesis
2. Inhibit protein synthesis
3. Inhibit nucleic acid synthesis
4. Injury to plasma membrane
5. Inhibit synthesis of essential metabolites

3. Figure 20.2

4. C. DRUG PROFILE OF ATLEAST 25 IMPORTANT MEDICATIONS
AMINOGLYCOSIDES
Protein synthesis inhibitors (Amikacin, Gentamicin,
Neomycin, Streptomycin, Tobramycin)
Aminoglycoside antibiotics had been the mainstays for
treatment of serious infections due to aerobic gram-
negative bacilli.
However, because their use is associated with serious
toxicities, they have been replaced to some extent by safer
antibiotics, such as the third- and fourth-generation
cephalosporins, the fluoroquinolones etc.
NOTE: Aminoglycosides that are derived from Streptomyces
have -mycin suffixes, whereas those derived from
Micromonospora end in -micin.

5. C. DRUG PROFILE OF ATLEAST 25 IMPORTANT MEDICATIONS
AMINOGLYCOSIDES….1
PHARMACOKINETICS
ADMINISTRATION
 Aminoglycosides are highly polar drugs (polycationic drugs).
These are not absorbed from GIT; So they are administered
parenterally
 EXCEPT Neomycin which should not be given parenterally, it
should be administered tropically.
EXCRETION
 Aminoglycosides are excreted in urine as such and most of them
are Nephrotoxic drug.
 The excretion is reduced in renal diseases.

6. C. DRUG PROFILE OF ATLEAST 25 IMPORTANT MEDICATIONS
AMINOGLYCOSIDES….1
PHARMACODYNAMICS
MECHANISM OF ACTION
 Aminoglycosides mainly acts on 30 S ribosomal subunit of RNA;
Which will lead to misreading of genetic code so the wrong
amino acid will incorporate to the peptide chain.
 So the protein which are formed will not be according to the
demand of bacteria.

7. Figure 20.4b

8. C. DRUG PROFILE OF ATLEAST 25 IMPORTANT MEDICATIONS
AMINOGLYCOSIDES….1
INDICATIONS
 Respiratory tract infections.
 Urinary tract infections
 Meningitis (Streptomycin)
 For tropical infections
 Brucellosis (Brucella, transmitted to humans from lower animals,
especially cattle, dogs, and goats. Human beings acquire the disease
through contact with infected animals or by drinking their raw milk)
 Endocarditis
 Infected burns
 Pneumonia
 Sepsis

9. C. DRUG PROFILE OF ATLEAST 25 IMPORTANT MEDICATIONS
AMINOGLYCOSIDES….1
CONTRAINDICATIONS
 Pregnancy (causes damaged of 8th Cranial Nerve vestibulo
cochlear nerve of fetus which causes deafness) .
 Mysthenia Gravis (Weakness of muscle because of
Neuromuscular blockade)
ADVERSE DRUG REACTION
 Ototoxicity (due to destruction of 8th cranial nerve
 Nephrotoxicity (due to the destruction of tubular cells of the
nephron) Neomycine and Gentamycine.
 Neurotoxicity (due to neuromuscular blockade because of the
inhibition of the release of acetylcholine).
 Hypersensitivity reactions like dermatitis

10. C. DRUG PROFILE OF ATLEAST 25 IMPORTANT MEDICATIONS
AMINOGLYCOSIDES….1
DRUG-DRUG INTERACTIONS
 Those drugs which are nephrotoxic interacts with
aminoglycosides and causes nephrotoxicity e.g. Furosimide and
Ethacrynic acid
 It potentiate the effect of Neuromuscular blocking drugs e.g.
Tubucurarine and Hexamethonium.
 If aminoglycosides are combined with penicilline its anti-
bacterial activity enhances.
DOSAGE FORM
 Injectable
 Topical preparation (Neomycin)

11. C. DRUG PROFILE OF ATLEAST 25 IMPORTANT MEDICATIONS
AMINOGLYCOSIDES….1
BRANDS
Gentamycin (Dose: 3-5 mg/Kg body weight for 7 days)
 Cidomycin (Aventis) Injection 20, 80, 120 mg
 Gentycin (Ricket) Injection 40, 80 mg
 Refobacin (Merck) Injection 10,20,40,80 mg
Kenamycin (Dose: 15 mg/kg body weight)
 Kanamycin (Zafa) Injection 500, 1000 mg
 Wege (Mass Pharma) Injection 500, 1000 mg
Amikacin (Dose: 15 mg/Kg body weight)
 Gracil (Sami) Injection 25, 50, 100, 250, 500 mg
 Amikacin (Zafa) Injection 100, 250, 500 , 1000 mg